|Targets||Orexin Receptor (OX Receptor)|
|Description||Filorexant, a selective reversible and orally bioavaliable antagonist of OX(1)R receptor and OX(2)R receptor, could probably be an effective compound in the treatment of insomnia. It is still under the Phase II trial by Merck. Binding Ki: less than 3 nM.|
|Synonyms||FILOREXANT; MK-6096; UNII-E6BTT8VA5Z; MK6096; MK 6096|
|Solubility||10 mM in DMSO|
|Application||Filorexant, a selective reversible and orally bioavaliable antagonist of OX(1)R receptor and OX(2)R receptor, could probably be an effective compound in the treatment of insomnia.|
|Shelf Life||As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly|
|Current Developer||Merck & Co|
SB-674042 is potent and selective non-peptide orexin OX1 receptor antagonist (Kd = 3.76 nM), by binding with high affinity to OX1R and mediates intracellular ca...
IPSU is a selective, orally available and brain penetrant OX2 receptor antagonist (pKi= 7.85) with 6-fold selectivity over OX1 receptors.
SB-408124 (Hydrochloride) is the hydrochloride salt form of SB-408124. SB-408124 is a selective antagonist of OX1 (for human OX1 Kb= 21.7nM; for human OX2 Kb=14...
SB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2.
TCS 1102 is a potent, dual orexin receptor antagonist with Ki values of 0.2 and 3 nM for OX2 and OX1 receptors respectively. It is a poor substrate for P-glycop...
TCS-OX2-29, also known as TCSOX229, is a selective OX2 receptor antagonist (IC50 = 40 nM, pKi = 7.5) with >250-fold selectivity for hOX2R compared with hOX1R (I...
Almorexant HCl is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and OX2, re...
SB-334867, with sedative and anorectic effects, it is the first non-peptide selective antagonist of orexin receptor subtype OX1 (pKb= 7.2) with 50 -fold selecti...
Lemborexant, an orexin OX1/OX2 receptors antagonist, has been found to be effective against insomnia and is just planed a Phase III trail by Eisai.
SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity ove...
Orexin 2 Receptor Agonist
N-[2-[3-[[5-[3-(dimethylcarbamoyl)phenyl]-2-methoxyphenyl]sulfonylamino]anilino]ethyl]-3-methylbenzamide is an orexin 2 receptor agonist that is potentially for...
Almorexant(ACT078573) is a potent and competitive dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist with Ki values of 1.3 and 0.17 nM for OX1 and ...
MK3697 is a highly potent, orally bioavailable selective orexin 2 receptor antagonists (2-SORAs) that possess acceptable profiles for clinical development. MK-3...
Filorexant, a selective reversible and orally bioavaliable antagonist of OX(1)R receptor and OX(2)R receptor, could probably be an effective compound in the tre...
JNJ-10397049 is a selective orexin-2 receptor (OX2) antagonist. pIC50 is 7.4 for chimeric OX2 receptors/ pKB values are 5.9 for OX1 and 8.5 for OX2 receptors re...
SB-649868 is a novel, orally active dual orexin receptor antagonist of orexin(OX)1 and OX2 receptor (pKi=9.4 and 9.5 at the OX1 and OX2 receptor, respectively),...